Nebivolol in the management of essential hypertension - A review

Nebivolol is a lipophilic beta(1)-blocker. It is devoid of intrinsic sympat homimetic or membrane stabilising activity but :appears to have nitric oxid e-mediated vasodilatory effects. Nebivolol is administered as a. racemic mi xture of equal proportions of d- and l-enantiomers. The drug does not signi ficantly influence glucose or plasma lipid metabolism and appears to have a protective effect on left ventricular function. At the recommended dosage (5 mg once daily) nebivolol reduces resting diast olic blood pressure as effectively as standard therapeutic dosages of ateno lol, metoprolol, lisinopril and nifedipine, as shown in comparative trials. Nebivolol reduced blood pressure significantly more than enalapril 10 mg d aily in the short but not the long term, although the enalapril dose may no t have been optimal. Nebivolol has on additive effect in combination with h ydrochlorothiazide. Standing blood pressure and/or mean 24-hour ambulatory blood pressure is significantly and similarly reduced with nebivolol, ateno lol or nifedipine. Nebivolol tended to prevent increases in early morning b lood pressure better than nifedipine. Overall response rates to nebivolol therapy (a decrease in sitting/supine d iastolic blood pressure to less than or equal to 90 mm Hg or a 10% or great er than or equal to 10 mm Hg fall in diastolic blood pressure) ranged from 58 to 81% after, 4 to 52 weeks treatment. In comparative studies, response rates were greater in nebivolol than in enalapril or metoprolol recipients, but not significantly different from those in atenolol or nifedipine recip ients. Nebivolol 5 mg once daily is well tolerated in patients with hypertension. adverse events we infrequent, transient and mild to moderate. Those reporte d most often include headache, fatigue paraesthesias and dizziness. Several studies reported no signs of orthostatic hypotension with nebivolol. Comparative trials revealed no significant differences between the frequenc y and severity of adverse events in patients receiving nebivolol, atenolol, enalapril or placebo: however, the overall incidence of adverse events was greater with nifedipine or metoprolol. Some atenolol or enalapril, but not nebivolol, recipients reported impotence or decreased libido during therap y. Conclusion: Current evidence indicates that nebivolol 5 mg once daily is a well tolerated beta-blocker, which is as effective as once daily atenolol a nd other classes of antihypertensive agents. It may therefore be recommende d as a useful alternative first-line treatment option for the management of patients with mild to moderate uncomplicated essential hypertension.